A general simple procedure having the potential for large scale preparations of racemic β3-amino acids has been developed. The procedure involves base-catalyzed Michael-type addition of sodium diethyl malonate to N-Boc-α-amidoalkyl-p-tolyl sulfones in tetrahydrofuran. Hydrolysis of the adducts by refluxing with 6 M aqueous hydrochloric acid affords β3-amino acid hydrochlorides in high yield and excellent purity.
Nejman, Micha?,?liwińska, Anna,Zwierzak, Andrzej
p. 8536 - 8541
(2007/10/03)
3,3,3-TRIFLUORO-2-MERCAPTOMETHYL-N-TETRAZOLYL SUBSTITUTED PROPANAMIDES AND METHOD OF USING SAME
Compounds of the formula STR1 wherein Y can be tetrazolyl are disclosed. These compounds are useful as cardiovascular agents.
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(2008/06/13)
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